《生命科学》 2012, 24(10): 1141-1150

大电导钙激活钾通道(BKCa)及其开放剂研究进展

王鹤云，吕遐师，林海霞，崔永梅^*

(上海大学理学院化学系，上海 200444)

摘　要：

摘　要：大电导钙激活钾通道(BKCa)广泛分布在哺乳动物各种组织(不含心肌细胞)中，并参与细胞内信号转导、细胞的兴奋及代谢调节等生理过程。BKCa功能异常牵涉到特发性癫痫、高血压等疾病的发生。BKCa通道是治疗高血压、尿失禁、哮喘、冠心病及缺血性脑中风等疾病的潜在药物靶点。探索高活性、高选择性、细胞通透性优良、类药性好的BKCa通道开放剂，不仅有助于阐明BKCa通道在生理病理条件下的作用机制，而且为治疗心脑血管疾病的药物研发奠定基础。对各类BKCa通道开放剂做一概述。

    

关键词：大电导钙激活钾通道；开放剂；药物

    

中图分类号：Q424；R966；R972  文献标志码：A

Progress in the studies of large-conductance calcium-activated potassium channel openers

WANG He-Yun， LÜ Xia-Shi， LIN Hai-Xia， CUI Yong-Mei^*

(Department of Chemistry， Shanghai University， Shanghai 200444， China)

Abstract:

Abstract: Large-conductance calcium-activated potassium channels (BKCa channels) are widely expressed in various cells and tissues of mammals except myocardial cells， and participate in many physiological processes， such as intracellular signal transduction， cellular excitability and metabolic regulation. The dysfunction of BKCa channels is related to the occurrence of idiopathic epilepsy， hypertension and many other diseases. BKCa channels are potential drug targets for the treatment of hypertension， urinary incontinence， asthma， coronary heart disease and ischemic stroke， et al. Exploring BKCa channel openers with high activity， high selectivity， excellent cell permeability and good drug-likeness will not only help to elucidate the mechanism of action of BKCa channels in physiological and pathological conditions， but also lay the foundation for the drug researches on the treatment of cardiovascular and cerebrovascular diseases. This paper mainly reviews the various types of BKCa channel openers.

    

Key words: BKCa channel; BKCa channels open agent; drug